Key Points

• Biktarvy (bictegravir, tenofovir, and emtricitabine) is not FDA approved for use as an HIV-1 preventive for pre-exposure prophylaxis (PrEP) or as a post-exposure prophylaxis (PEP) treatment. Biktarvy is used for HIV treatment (not for prevention) as a once-daily, oral complete regimen.
• Medications approved by the FDA for use in PrEP are emtricitabine plus tenofovir alafenamide (oral Descovy), emtricitabine plus tenofovir disoproxil (oral Truvada) or the long-acting injection cabotegravir (Apretude).
• The recommended options for PEP in adults includes tenofovir and emtricitabine (Truvada), plus either raltegravir (Isentress) or dolutegravir (Tivicay), given as a 28-day treatment.

PrEP and PEP are effective regimens used to prevent HIV infection. However, Biktarvy is not approved for use as an agent for HIV prevention (PrEP) or for emergency use in case of an HIV exposure in an HIV-negative person (PEP). Biktarvy is used for treatment of HIV-1 infection (not prevention).

• PrEP is the use of an antiretroviral medication for people who are HIV-negative and at substantial risk for HIV infection, including high-risk men who have sex with men; high-risk heterosexual men and women; and high-risk injection drug users.
• PEP is the use of an antiretroviral medication to lower your risk of becoming HIV-positive if you have been exposed to HIV and it is less than 72 hours since your exposure.

How is Biktarvy used in HIV treatment?

In February 2018, the FDA approved Biktarvy (bictegravir, emtricitabine and tenofovir alafenamide, often abbreviated BIC/FTC/TAF) from Gilead Sciences.

Biktarvy contains an integrase strand transfer inhibitor (bictegravir) and the non-nucleoside reverse transcriptase inhibitor (NNRTI) emtricitabine and tenofovir alafenamide (Descovy) combination for the treatment of HIV-1 infection in adults. It works by preventing HIV viral replication in the cell.

It is a complete, once-daily, single tablet regimen for the treatment of two HIV groups: either those who have no antiretroviral treatment history or those who are already virologically suppressed on another stable HIV regimen with no history of treatment failure or known resistance.

Biktarvy is for use in adults and children who weigh at least 31 pounds (14 kilograms). Biktarvy is not a cure for HIV or AIDS.

How well does Biktarvy work to treat HIV?

Adults

In Phase 3 studies of over 2,400 participants, Biktarvy met the study endpoint of proportion of adults with HIV-1 RNA <50 copies/mL at Week 48. Results were non-inferior (meaning Biktarvy effectiveness was not found to be worse than the active controls) at 48 weeks across all four groups.

In one study, treatment-naïve adults receiving Biktarvy once daily were compared to those receiving FTC/TAF + DTG (Descovy plus Tivicay).

• At week 48, 92% of patients receiving Biktarvy had HIV-1 RNA < 50 copies per mL (considered undetectable) as compared to 93% receiving FTC/TAF + DTG, a value considered non-inferior.
• Biktarvy taken once a day was studied in patients who were already virologically suppressed on another stable, once-daily HIV regimen (ABC/DTG/3TVC, or brand name Triumeq), At least 92% of adults who switched to Biktarvy maintained virologic suppression at Week 48.
• In addition, among treatment-naïve and virologically-suppressed adults in 5 studies, no amino acid substitutions emerged that were associated with Biktarvy resistance through Week 144 for treatment-naïve patients and through Week 48 in virologically-suppressed adults.

Children (14 kg to less than 25 kg)

In October 2021, the FDA approved a new low-dose tablet formulation of Biktarvy (bictegravir 30 mg/emtricitabine 120 mg/tenofovir alafenamide 15 mg tablets) for pediatric patients weighing at least 14 kg to less than 25 kg. In virologically suppressed children living with HIV-1 and weighing at least 14 kg, Biktarvy low-dose tablets were found to be effective and well-tolerated.

• After switching to Biktarvy, 91% (20/22) of participants remained virologically suppressed at Week 24 (HIV-1 RNA < 50 copies/mL). The mean change in CD4 % from baseline was 0.2%
• HIV-1 RNA data from two participants was not collected at Week 24 because of COVID-19 pandemic-related study disruption.
• In pediatric studies, no new adverse reactions or laboratory abnormalities were identified compared to adults.

Biktarvy does not require testing for HLA-B5701 (unlike abacavir), can be taken with or without food, and has no baseline viral load or CD4 count restrictions.

The most common side effects of Biktarvy are diarrhea (occurring in about 6% of patients), nausea (5%), and headache (5%).

Biktarvy has many serious drug interactions. Do not use Biktarvy with:

• dofetilide (Tikosyn), a drug used for irregular heartbeats
• rifampin (Rifadin), a medicine for treating tuberculosis (TB)

Always check with your doctor or pharmacist for potential Biktarvy drug interactions with your medications, including prescription medicines, over-the-counter, herbal or dietary supplements.

HIV Prevention with Truvada or Descovy

PrEP can lower your chances of contracting HIV from sex by up to 99%, if used correctly.

In July 2012 the FDA approved the use of Gilead’s Truvada, an antiretroviral medication for PREP to prevent HIV infection in certain high-risk individuals.

Truvada is a two-drug tablet that contains tenofovir disoproxil fumarate plus emtricitabine and can be used in high-risk, HIV-negative persons to lower their risk of infection. For many years, Truvada was the only approved option for PrEP.

However, in October 2019, the FDA also approved Descovy (emtricitabine and tenofovir alafenamide) as the second drug for PrEP.

• Descovy is used in at-risk, HIV-1 negative adults and adolescents weighing at least 35 kg to reduce the risk of sexually acquired HIV-1 infection.

• Descovy is not approved for use in people assigned female at birth (cisgender) who are at risk of getting HIV from vaginal sex, because its effectiveness has not been fully evaluated in clinical studies.

In studies, Descovy was as effective as Truvada in HIV-1 prevention, but advantages were observed with regard to renal (kidney) and bone laboratory secondary endpoints.

Apretude: A long-acting PrEP injection

In Dec. 2021, ViiV Healthcare's long-acting Apretude injection was cleared for HIV PrEP. Apretude is classified as an integrase strand transfer inhibitor (INSTI). Apretude is approved for use in adults and adolescents weighing at least 35 kg (77 lb).

• Apretude is given as a gluteal (buttocks) intramuscular injection once a month for the first 2 months, then once every 2 months by a healthcare provider. A negative HIV test is required prior to each injection.
• Before the first Apretude injection, patients may take oral cabotegravir (Vocabria) for at least 28 days to determine cabotegravir tolerability (this is not required). However, no safety and efficacy data are available for use of Apretude without use of Vocabria first.

Common side effects with Apretude included injection site reactions (primarily pain/tenderness), diarrhea, headache, fever (pyrexia), fatigue, sleep disorders, nausea, dizziness, flatulence, and abdominal (stomach area) pain.

PrEP Tips

• You must take oral PrEP medication daily. It's important not to miss any doses to help prevent resistance to these medications.
• Use PrEP in combination with safe sex practices such as use of a condom.
• Everyone is screened for HIV-1 infection before initiating PrEP. You must be HIV-1 negative to start PrEP.
• Regular tests for HIV status are required with PrEP.

HIV Post-Exposure Prophylaxis (PEP)

PEP stands for post-exposure prophylaxis. Post-exposure prophylaxis means you would take HIV medicines within 72 hours after a possible exposure to HIV to help prevent becoming infected with HIV. You might also need PEP if or have missed taking your PrEP as prescribed.

The sooner you get medical care, the better. PEP has limited effect in preventing HIV infection if you do not start treatment within 72 hours after potential HIV exposure.

You may be eligible for PEP:

• If you were exposed to HIV during sex (for example, a condom broke or no condom was used).
• If you were exposed to HIV by sharing needles, syringes or other IV drug use materials (“works”).
• If you’ve been sexually assaulted.
• If you're a healthcare worker exposed to HIV.

The CDC recommends the following regimens for PEP:

• For adults, use three drugs: tenofovir and emtricitabine (found in Truvada) and raltegravir (Isentress) or dolutegravir (Tivicay).
• A PEP regimen is taken once or twice a day for 28 days. PEP is effective in preventing HIV when administered correctly, but it is not always 100% effective.

A small but significant increase in neural tube defects (NTDs) was observed following maternal use of dolutegravir (DTG) in one study.

• Alternative treatments to DTG should be considered at the time of conception through the first trimester of pregnancy due to the risk of neural tube defects.
• Decisions about DTG use should be made after discussing the risks and benefits with the patient and following the most recent guidelines.
• CDC currently recommends that prior to starting PEP all women of childbearing potential should have a pregnancy test performed. Women of childbearing potential should use effective contraception when using DTG.

PEP is used only in emergency situations and is not a regular substitute for proven HIV prevention measures, such as PrEP, condom use, and safe needle practices.

Bottom Line

• Biktarvy is used to treat someone living with an HIV-1 infection. It is not used to prevent HIV-1 infection in PrEP or PEP.
• The dose of Biktarvy is one tablet taken once a day with or without food in adults and children who weigh at least 14 kg (31 lb).
• In studies looking at Biktary for HIV treatment, most patients were able to reach an undetectable level of virus in their blood with Biktarvy (fewer than 50 copies of HIV per milliliter of blood).
• Biktarvy is usually well-tolerated. The most common side effects include diarrhea (6% of patients), nausea (5%), and headache (5%).

This is not all the information you need to know about Biktarvy for safe use. Review the full Biktarvy information here, and review this information with your health care provider.